Human steroid receptor
    1.
    发明授权
    Human steroid receptor 失效
    人类类固醇受体

    公开(公告)号:US5939322A

    公开(公告)日:1999-08-17

    申请号:US646248

    申请日:1996-05-14

    摘要: Through the use of the novel receptor NER in a screening procedure, TOFA (5-tetradecyloxy)-2-furan-carboxylic acid) has been found to modulate other receptors and to be a potent potentiator of other drugs. TOFA activates the NER receptor. The NER receptor is a novel member of the steroid hormone receptor family and has been prepared by cDNA cloning from a human osteosarcoma SAOS-2/B10 cell library. Also disclosed is the complete sequence of human NER cDNA; a COS stable expression system; the expressed NER protein; and an assay using the COS expression system. In addition, the invention relates to a method for identifying functional ligands of the NER receptor.

    摘要翻译: PCT No.PCT / US95 / 13924 Sec。 371日期:1996年5月14日 102(e)日期1996年5月14日PCT提交1995年10月24日PCT公布。 第WO96 / 13519号公报 日期1996年5月9日通过在筛选程序中使用新型受体NER,已经发现TOFA(5-十四烷氧基)-2-呋喃羧酸)调节其他受体并成为其他药物的有效增强剂。 TOFA激活NER受体。 NER受体是类固醇激素受体家族的新成员,并通过人骨肉瘤SAOS-2 / B10细胞库的cDNA克隆制备。 还公开了人NER cDNA的完整序列; COS稳定表达系统; 表达的NER蛋白; 和使用COS表达系统的测定法。 另外本发明涉及一种鉴定NER受体功能性配体的方法。

    Human protein tyrosine phosphatase OB protein
    3.
    发明授权
    Human protein tyrosine phosphatase OB protein 失效
    人蛋白酪氨酸磷酸酶OB蛋白

    公开(公告)号:US5866397A

    公开(公告)日:1999-02-02

    申请号:US800825

    申请日:1997-02-14

    CPC分类号: C12Q1/42

    摘要: A novel human protein tyrosine phosphatase (PTP) has been identified and its cDNA has been isolated. This novel PTP, denoted PTP-OB, has a receptor-like three dimensional structure and is present in osteoblasts. PTP-OB is involved in osteoblast differentiation, and modulators of PTP-OB activity in turn modulate osteoblast differentiation, osteoclast differentiation and osteoclast activity.

    摘要翻译: 已经鉴定出新的人蛋白酪氨酸磷酸酶(PTP),并且已经分离了其cDNA。 这种新型PTP,表示为PTP-OB,具有受体样三维结构,并存在于成骨细胞中。 PTP-OB参与成骨细胞分化,PTP-OB活性的调节剂又调节成骨细胞分化,破骨细胞分化和破骨细胞活性。

    Method of identifying modulators of protein tyrosine phosphatase activity
    6.
    发明授权
    Method of identifying modulators of protein tyrosine phosphatase activity 失效
    识别蛋白酪氨酸磷酸酶活性调节剂的方法

    公开(公告)号:US06214564B1

    公开(公告)日:2001-04-10

    申请号:US09158657

    申请日:1998-09-22

    IPC分类号: G01N3353

    CPC分类号: C12Q1/42

    摘要: A human protein tyrosine phosphatase (PTP) has been identified and its cDNA has been isolated. This PTP, denoted PTP-OB, has a receptor-like three dimensional structure and is present in osteoblasts. PTP-OB is involved in osteoblast differentiation, and modulators of PTP-OB activity in turn modulate osteoblast differentiation, osteoclast differentiation and osteoclast activity.

    摘要翻译: 已经鉴定出人蛋白质酪氨酸磷酸酶(PTP),并且已经分离了其cDNA。 该PTP(表示为PTP-OB)具有受体样三维结构并且存在于成骨细胞中。 PTP-OB参与成骨细胞分化,PTP-OB活性的调节剂又调节成骨细胞分化,破骨细胞分化和破骨细胞活性。

    Androgen receptor modulators and methods for use thereof
    8.
    发明授权
    Androgen receptor modulators and methods for use thereof 失效
    雄激素受体调节剂及其使用方法

    公开(公告)号:US06645974B2

    公开(公告)日:2003-11-11

    申请号:US10205634

    申请日:2002-07-25

    IPC分类号: A61K3158

    摘要: Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of agonizing the androgen receptor in a patient, and in particular the method wherein the androgen receptor is antagonized in the prostate of a male patient or in the uterus of a female patient and agonized in bone and/or muscle tissue. These compounds are useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including: osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, arthritis and joint repair, alone or in combination with other active agents. In addition, these compounds are useful as pharmaceutical composition ingredients alone and in combination with other active agents.

    摘要翻译: 公开了本文定义的结构式(I)的化合物可用于在需要这种调节的患者中以组织选择性方式调节雄激素受体的方法,以及在患者中激动雄激素受体的方法 ,特别是其中雄性受体在男性患者的前列腺或女性患者的子宫中被拮抗并在骨和/或肌肉组织中激动的方法。 这些化合物可用于治疗由雄激素缺乏引起的或可由雄激素施用而改善的病症,包括:骨质疏松症,牙周病,骨折,骨重建手术后的骨损伤,肌肉减少症,虚弱,衰老皮肤,男性性腺机能减退 妇女的绝经症状,动脉粥样硬化,高胆固醇血症,高脂血症,再生障碍性贫血和其他造血障碍,胰腺癌,肾癌,关节炎和关节修复,单独或与其他活性剂组合。 此外,这些化合物可单独用作药物组合物成分并与其它活性剂组合使用。